1. Technical Field
The present invention relates, in general, to an injectable composition for local administration for treating hemorrhoids, which contains hydroxychloroquine, and more particularly to an injectable composition for treating hemorrhoids, which is to be injected directly into the hemorrhoidal area to harden the hemorrhoidal tissue so as to block metabolism in the hemorrhoidal tissue, thereby inactivating the hemorrhoidal tissue, and ultimately necrotizing the hemorrhoidal tissue.
2. Description of the Related Art
Hemorrhoids are the first leading cause of hospitalization in Korea, and 50% or more of people in their 50s or older suffer from these diseases (the Seoul National University Hospital). Also, about 50 of the USA population suffers from these diseases.
Generally, hemorrhoidal diseases which are the so-called hemorrhoids include hemorrhoids, anal fissure, perianal tumors, anal fistula, and show major symptoms, including bleeding, prolapse, pain, itching, rectal dysfunction, and soiling. Among them, the term “hemorrhoids” is most frequently used.
Hemorrhoids occur due to the stretching and expansion of vascular tissue beneath the skin and mucus tissue of the anal and are masses caused by stretching of the skin and mucosa covering the anal blood vessels. Hemorrhoids are classified into internal hemorrhoids, external hemorrhoids, and mixed hemorrhoids. Hemorrhoids occurring above the dentate line (approximately 1.5 cm above the inner verge of the anus dilator) are referred to as internal hemorrhoids; hemorrhoids occurring below the dentate line are referred to as external hemorrhoids; and hemorrhoids occurring both above and below the dentate line are referred to as mixed hemorrhoids. In the initial stage, there are only internal or external hemorrhoids, but in many cases, the internal or external hemorrhoids progress to mixed hemorrhoids with the passage of time.
The degree of progression of internal hemorrhoids is divided according to the degree of protrusion of hemorrhoids from the anus into: stage 1 in which a hemorrhoid is diagnosed due to bleeding, but the hemorrhoid does not protrude from the anus; stage 2 in which the hemorrhoid protrudes during bowel evacuation, but it returns to its original position immediately after bowel evacuation; stage 3 in which the hemorrhoid protrudes during bowel evacuation, and the protruded hemorrhoid returns to its original position a significant amount of time after bowel evacuation or returns by thrusting or lying down; and stage 4 in which the hemorrhoid that protruded during bowel evacuation does not easily returns to its original position or protrudes again immediately after return to its original position.
The degree of progression of external hemorrhoids is not objectively divided or can be divided based on the period of occurrence of thrombosis in view of the balance with internal hemorrhoids. Specifically, a stage-1 external hemorrhoid is referred to when thrombosis occurs and is swollen for less than 10 days per year; a stage-2 external hemorrhoid is referred to when thrombosis occurs and is swollen for about 11-20 days per year; a stage-3 external hemorrhoid is referred to when thrombosis occurs and is swollen for more than 3 weeks per year; and a stage-4 external hemorrhoid is referred to when thrombosis frequently occurs.
General methods for treating such hemorrhoids include: a method of suppressing bleeding of internal hemorrhoids; a method of suppressing thrombosis in external hemorrhoids and the resulting edema and pain; administration of internal medicines or suppositories; and sitz bath.
Internal medicines for treating hemorrhoids are based on blood circulation-improving agents and include about 10 commercially available medicinal products. Suppositories for treating hemorrhoids are composed of components having pain-killing, anti-inflammatory, antibacterial and astringent effects and include about 20 commercially available medicinal products.
As ointments and suppositories for treating hemorrhoids, formulations containing local anesthetics, steroidal agents and antihistamine agents are mainly used. Administration of the local anesthetics or steroidal agents alleviates temporary discomfort, but it delays wound healing and is highly likely to cause a variety of systemic and local side effects. Furthermore, administration of non-steroidal anti-inflammatory agents around a wound is prohibited, because it delays the treatment of disease.
In addition, surgical methods are avoided by patients and frequently fail to remove the root of hemorrhoids, because these methods remove only the protruding portion of hemorrhoids.
Korean Patent Laid-Open Publication No. 10-2005-0102663 discloses an agent for external application for treating hemorrhoids and anal fissure, which comprises acetylsalicylic acid or its salt as an active ingredient.
Korean Patent Registration No. 10-0863758 discloses a pharmaceutical composition for local application for treating acute or chronic anal fissure, thrombotic internal or external hemorrhoids and hemorrhoidal diseases, the composition containing an adenosine receptor antagonist selected from the group consisting of theophylline and dyphylline.
Korean Patent Laid-Open Publication No. 10-2008-0105857 discloses a composition for direct local application to surfaces, the composition containing a swellfish spawn extract, a swellfish liver extract, egg yolk oil and a Cnidium Rhizome extract and having activity of treating anal and rectal diseases.
However, an injectable composition for treating hemorrhoids containing hydroxychloroquine as disclosed in the present invention is not yet known, which is to be injected directly into the affected area to harden the hemorrhoidal tissue so as to block metabolism in the hemorrhoidal tissue, thereby inactivating the hemorrhoidal tissue, and ultimately necrotizing the hemorrhoidal tissue.